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. Author manuscript; available in PMC: 2022 Oct 14.
Published in final edited form as: ChemMedChem. 2022 Jun 14;17(15):e202000499. doi: 10.1002/cmdc.202000499

Table 2.

Piperidine hit series 2 SAR determined in the human sperm calcium influx assay

graphic file with name nihms-1812278-t0016.jpg
Compound R1 R2 IC50, μM
2a graphic file with name nihms-1812278-t0017.jpg Cl 7.5 ± 1.3
2b graphic file with name nihms-1812278-t0018.jpg H 92 ± 14
2c graphic file with name nihms-1812278-t0019.jpg Cl 18 ± 2
2d graphic file with name nihms-1812278-t0020.jpg 18 ± 7
2e graphic file with name nihms-1812278-t0021.jpg Cl > 100
2f graphic file with name nihms-1812278-t0022.jpg Cl > 100
2g graphic file with name nihms-1812278-t0023.jpg Cl > 100
2h graphic file with name nihms-1812278-t0024.jpg Cl > 100*
2i graphic file with name nihms-1812278-t0025.jpg Cl > 100*
2j graphic file with name nihms-1812278-t0026.jpg Cl 87*
2k graphic file with name nihms-1812278-t0027.jpg > 100*
2l graphic file with name nihms-1812278-t0028.jpg > 100*

CatSper activated by 3 μM progesterone. IC50 values are means ± SEM of 3 independent experiments.

*

IC50 values are means of 2 independent experiments.